PREPARATION AND CHARACTERIZATION OF NANOSTRUCTURED LIPID CARRIERS OF ANTINEOPLASTIC AGENTS

Abstract

The aim of this study was to prepare and characterize folic acid conjugated nanostructure lipid carriers (NLCs) as nanocarriers for parenteral delivery of gemcitabine (GEM) and paclitaxel (PTX). Folic acid-conjugated GEM-PTX-NLCs were prepared by solvent emulsion-evaporation method and characterized for particle size, polydispersity index and zeta potential which were found to be 134.62±4.11 nm, 0.189±0.05, +28.4±0.6 mV, respectively. Percent entrapment efficiency of GEM and PTX in FA-conjugated GEM-PTX- NLCs were recorded as 89.1±0.6 % and 86.6±0.8 % respectively, which was within an acceptable range for injectable formulation. In vitro drug release study of optimized formulation was carried out using the dialysis tube method. FA-conjugated GEM-PTX-loaded NLCs showed cumulative drug release 78.6±0.93 % and 75.3±0.7 % of GEM and PTX respectively in 72 h in PBS pH 7.4: methanol (7:3) while FA-conjugated GEM-PTX- NLCs showed cumulative drug release 85.5±0.075% and 82.2±0.72% of GEM and PTX respectively in 72 h in PBS pH 4.0 : methanol (7:3). Furthermore, stability testing data indicated that NLCs formulations stored at 5˚C±3˚C were more stable than those stored at 25˚C±2˚C/60% RH ± 5% RH. These results suggest that folic acid-conjugated GEM-PTX- NLCs have the potential for serving as a novel carrier system for delivery of antineoplastic agents.